摘要
目的:制备羧甲基壳聚糖包衣尼莫地平纳米脂质体,并对其进行体外释药考察。方法:采用薄膜分散法制备尼莫地平脂质体,并用不同浓度的羧甲基壳聚糖包衣,经高压均质机多次乳匀得到羧甲基壳聚糖包衣尼莫地平纳米脂质体。以包封率为指标,筛选最佳处方;用激光粒度分析仪测定其Zeta电位,粒径大小及分布,并用透射电镜观察其形态;用透析法考察其体外释药性质。结果:羧甲基壳聚糖与脂材比例为1:4制备得到的脂质体包封率最高,平均为(75.2±3.1)(n=3);Zeta电位为(-9.3±1.2)mV,平均粒径为(85.7±8.2)nm,(n=3);体外释药曲线符合Higuchi方程:Q=-0.1926+0.3579t1/2,(r=0.9800)。结论:本实验制备的羧甲基壳聚糖包衣尼莫地平纳米脂质体具有包封率高,粒径小,大小均匀,体外能显著延缓药物释放的性质,值得进一步研究。
OBJECTIVE To prepare carboxymethyl chitosan （CMC）-coated nimodipine nanoliposomes and study on their release in vitro. METHODS Nimodipine liposomes were prepared by the film dispersion method. CMCs with different concentrations were used to coat the liposomes followed by extruded through high pressure homogenizer to get nanoliposomes. The encapsulation efficiency was chosen as index to screen the optimal formulation of the preparation. The zeta potential, average size and size distribution were determined by Zetersizer. Dialyzer was employed to study the release of nimodipine from the nanoliposomes in vitro. REULTS The optimal encapsulation efficiency of the nanoliposomes was （75.18 ± 3. 13）% （n = 3） when the ratio of CMC to lipid was 1：4. The Zeta potencial of CMC coated nimodipine nanoliposomes was （ - 9. 28 ± 1.23）mV and average size was （85.7 ± 8. 25）nm （n = 3）. The drug release in vitro was accorded with the Higuchi equation： Q= - 0. 192 6 ＋ 0. 357 9t^1/2 （r = 0. 980 02）. CONCLUSION The CMC-coated nimodipine nanoliposomes with promising encapsulation efficiency, nanometeric sizes and delayed drug release in vitro were valuable to be studied further.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2008年第17期1463-1466,共4页
Chinese Journal of Hospital Pharmacy
